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maprotiline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	1634	10262-69-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: maprotiline maprotiline hydrochloride maprotiline HCl	A bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use. Molecular weight: 277.41 Formula: C20H23N CLOGP: 4.52 LIPINSKI: 0 HAC: 1 HDO: 1 TPSA: 12.03 ALOGS: -6.27 ROTB: 4 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

maprotiline
maprotiline hydrochloride
maprotiline HCl

A bridged-ring tetracyclic antidepressant that is both mechanistically and functionally similar to the tricyclic antidepressants, including side effects associated with its use.

Molecular weight: 277.41
Formula: C20H23N
CLOGP: 4.52
LIPINSKI: 0
HAC: 1
HDO: 1
TPSA: 12.03
ALOGS: -6.27
ROTB: 4

Status: OFM

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.10	g	O
0.10	g	P

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	68 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
t_half (Half-life)	51 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	45 L/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	3.13 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	3 %	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	14 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	11.59 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.11 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Dec. 1, 1980	FDA

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Polydipsia	60.41	33.02	14	1225	3550	63484233
Aspiration	49.21	33.02	15	1224	10836	63476947
Rhabdomyolysis	43.99	33.02	20	1219	43931	63443852
Mental disorder	39.87	33.02	16	1223	25903	63461880
Conjunctivitis	36.05	33.02	14	1225	20782	63467001
Embolic stroke	34.35	33.02	9	1230	3767	63484016

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FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Rhabdomyolysis	57.07	43.16	26	846	103105	79640411
Polydipsia	49.51	43.16	12	860	6593	79736923
Aspiration	44.45	43.16	14	858	20144	79723372

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N06AA21	NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Non-selective monoamine reuptake inhibitors
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D018759	Adrenergic Uptake Inhibitors
MeSH PA	D000928	Antidepressive Agents
MeSH PA	D018687	Antidepressive Agents, Second-Generation
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D014179	Neurotransmitter Uptake Inhibitors
MeSH PA	D011619	Psychotropic Drugs

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Depressive disorder	indication	35489007
Mixed anxiety and depressive disorder	indication	231504006
Neuralgia	off-label use	16269008
Ocular hypertension	contraindication	4210003	DOID:9282
Suicidal thoughts	contraindication	6471006
Alcoholism	contraindication	7200002
Sinus tachycardia	contraindication	11092001
Bipolar disorder	contraindication	13746004	DOID:3312
Myocardial infarction	contraindication	22298006	DOID:5844
Hyperthyroidism	contraindication	34486009	DOID:7998

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	9.91	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN	INHIBITOR	Kd	8.27	WOMBAT-PK	CHEMBL
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	6.18	WOMBAT-PK
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	6.17	DRUG MATRIX
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		IC50	5.36	DRUG MATRIX
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		Ki	5.24	PDSP
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	6.92	WOMBAT-PK
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	6.67	DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	7.39	DRUG MATRIX
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	6.38	DRUG MATRIX
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		IC50	9.85	WOMBAT-PK

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External reference:

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ID	Source
001510	NDDF
004608	NDDF
10347-81-6	SECONDARY_CAS_RN
10424009	SNOMEDCT_US
1567	MMSL
203126	RXNORM
2402	IUPHAR_LIGAND_ID
2763	INN_ID
2U1W68TROF	UNII
32823007	SNOMEDCT_US

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Pharmaceutical products:

None